Literature DB >> 15454221

Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones.

Anthony B Pinkerton1, Rowena V Cube, John H Hutchinson, Blake A Rowe, Hervé Schaffhauser, Xiumin Zhao, Lorrie P Daggett, Jean-Michel Vernier.   

Abstract

We have identified and synthesized a series of aryl-tetrazoyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation led to the discovery of 22 (EC(50)=93nM, 128% potentiation).

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Year:  2004        PMID： 15454221     DOI： 10.1016/j.bmcl.2004.08.020

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  Discovery of 1,5-disubstituted pyridones: a new class of positive allosteric modulators of the metabotropic glutamate 2 receptor.

Authors:  Jose María Cid; Guillaume Duvey; Philippe Cluzeau; Vanthea Nhem; Karim Macary; Alexandre Raux; Nicolas Poirier; Jessica Muller; Christelle Boléa; Terry Finn; Sonia Poli; Mark Epping-Jordan; Emilie Chamelot; Francis Derouet; Francoise Girard; Gregor J Macdonald; Juan Antonio Vega; Ana Isabel de Lucas; Encarnación Matesanz; Hilde Lavreysen; María Lourdes Linares; Daniel Oehlrich; Julen Oyarzábal; Gary Tresadern; Andrés A Trabanco; Jose Ignacio Andrés; Emmanuel Le Poul; Hassan Imogai; Robert Lutjens; Jean-Philippe Rocher
Journal:  ACS Chem Neurosci       Date:  2010-08-23       Impact factor: 4.418

Review 2.  Recent progress in the synthesis and characterization of group II metabotropic glutamate receptor allosteric modulators.

Authors:  Douglas J Sheffler; Anthony B Pinkerton; Russell Dahl; Athina Markou; Nicholas D P Cosford
Journal:  ACS Chem Neurosci       Date:  2011-04-12       Impact factor: 4.418

3.  Design and synthesis of an orally active metabotropic glutamate receptor subtype-2 (mGluR2) positive allosteric modulator (PAM) that decreases cocaine self-administration in rats.

Authors:  Raveendra-Panickar Dhanya; Shyama Sidique; Douglas J Sheffler; Hilary Highfield Nickols; Ananda Herath; Li Yang; Russell Dahl; Robert Ardecky; Svetlana Semenova; Athina Markou; P Jeffrey Conn; Nicholas D P Cosford
Journal:  J Med Chem       Date:  2010-12-14       Impact factor: 7.446

4.  The mGluR2 positive allosteric modulator BINA decreases cocaine self-administration and cue-induced cocaine-seeking and counteracts cocaine-induced enhancement of brain reward function in rats.

Authors:  Xinchun Jin; Svetlana Semenova; Li Yang; Robert Ardecky; Douglas J Sheffler; Russell Dahl; P Jeffrey Conn; Nicholas D P Cosford; Athina Markou
Journal:  Neuropsychopharmacology       Date:  2010-06-16       Impact factor: 7.853

5.  Metabotropic glutamate receptors: potential drug targets for psychiatric disorders.

Authors:  Akito Yasuhara; Shigeyuki Chaki
Journal:  Open Med Chem J       Date:  2010-05-27

6.  Improved synthesis of 5-substituted 1H-tetrazoles via the [3+2] cycloaddition of nitriles and sodium azide catalyzed by silica sulfuric acid.

Authors:  Zhenting Du; Changmei Si; Youqiang Li; Yin Wang; Jing Lu
Journal:  Int J Mol Sci       Date:  2012-04-12       Impact factor: 6.208

7.  Allosteric modulators for mGlu receptors.

Authors:  F Gasparini; W Spooren
Journal:  Curr Neuropharmacol       Date:  2007-09       Impact factor: 7.363

8.  Beyond dopamine: glutamate as a target for future antipsychotics.

Authors:  Kyra-Verena Sendt; Giovanni Giaroli; Derek K Tracy
Journal:  ISRN Pharmacol       Date:  2012-07-05

9.  Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): pharmacological characterization and assessment in a rat model of cocaine dependence.

Authors:  Raveendra-Panickar Dhanya; Douglas J Sheffler; Russell Dahl; Melinda Davis; Pooi San Lee; Li Yang; Hilary Highfield Nickols; Hyekyung P Cho; Layton H Smith; Manoranjan S D'Souza; P Jeffrey Conn; Andre Der-Avakian; Athina Markou; Nicholas D P Cosford
Journal:  J Med Chem       Date:  2014-05-09       Impact factor: 7.446
  9 in total

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